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Ligand-Induced Conformations Of Extracellular Loop 2 Of At1r, Hamiyet Unal

ETD Archive

Angiotensin II type 1 receptor (AT1R) is a G-protein coupled receptor (GPCR) and an important regulator of blood pressure. It is a target for drug development, because abnormalities in its function are linked to hypertension, cardiac hypertrophy and heart failure. AT1R is composed of seven transmembrane helices connected by three extracellular loops and three intracellular loops. The extracellular loop 2 (ECL2) of AT1R directly interacts with the ligands. This loop is targeted by autoantibodies that activate AT1R in several pathologies such as preeclampsia, malignant hypertension and vascular allograft rejection. Therefore, we proposed that the conformation of ECL2 in AT1R is …